CN102471313B - Gpr119激动剂 - Google Patents

Gpr119激动剂 Download PDF

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Publication number
CN102471313B
CN102471313B CN201080031375.4A CN201080031375A CN102471313B CN 102471313 B CN102471313 B CN 102471313B CN 201080031375 A CN201080031375 A CN 201080031375A CN 102471313 B CN102471313 B CN 102471313B
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CN
China
Prior art keywords
compound
methyl
methylsulfonyl
mixture
tetrahydrochysene
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Expired - Fee Related
Application number
CN201080031375.4A
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English (en)
Chinese (zh)
Other versions
CN102471313A (zh
Inventor
D·G·巴莱特
J·B·弗朗西斯科维奇
刘斌
K·塔克乌奇
A·B·布埃诺梅伦多
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Eli Lilly and Co
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Eli Lilly and Co
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Publication date
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First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=43449712&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=CN102471313(B) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Eli Lilly and Co filed Critical Eli Lilly and Co
Publication of CN102471313A publication Critical patent/CN102471313A/zh
Application granted granted Critical
Publication of CN102471313B publication Critical patent/CN102471313B/zh
Expired - Fee Related legal-status Critical Current
Anticipated expiration legal-status Critical

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Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/04Anorexiants; Antiobesity agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/06Antihyperlipidemics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings

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  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Diabetes (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Emergency Medicine (AREA)
  • Endocrinology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Hydrogenated Pyridines (AREA)
CN201080031375.4A 2009-07-15 2010-07-12 Gpr119激动剂 Expired - Fee Related CN102471313B (zh)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
EP09382114 2009-07-15
EP09382114.8 2009-07-15
US24544509P 2009-09-24 2009-09-24
US61/245,445 2009-09-24
PCT/US2010/041645 WO2011008663A1 (en) 2009-07-15 2010-07-12 Gpr119 agonists

Publications (2)

Publication Number Publication Date
CN102471313A CN102471313A (zh) 2012-05-23
CN102471313B true CN102471313B (zh) 2014-06-04

Family

ID=43449712

Family Applications (1)

Application Number Title Priority Date Filing Date
CN201080031375.4A Expired - Fee Related CN102471313B (zh) 2009-07-15 2010-07-12 Gpr119激动剂

Country Status (24)

Country Link
US (1) US8207344B2 (enExample)
EP (1) EP2454251A1 (enExample)
JP (1) JP5715127B2 (enExample)
KR (1) KR101365854B1 (enExample)
CN (1) CN102471313B (enExample)
AR (1) AR077638A1 (enExample)
AU (1) AU2010273642B2 (enExample)
BR (1) BRPI1015921A2 (enExample)
CA (1) CA2764906C (enExample)
CO (1) CO6480977A2 (enExample)
CR (1) CR20120012A (enExample)
DO (1) DOP2012000006A (enExample)
EA (1) EA020540B1 (enExample)
EC (1) ECSP12011606A (enExample)
IL (1) IL216776A0 (enExample)
MA (1) MA33428B1 (enExample)
MX (1) MX2012000704A (enExample)
NZ (1) NZ597125A (enExample)
PE (1) PE20121045A1 (enExample)
SG (1) SG177646A1 (enExample)
TN (1) TN2012000002A1 (enExample)
TW (1) TWI429634B (enExample)
WO (1) WO2011008663A1 (enExample)
ZA (1) ZA201200227B (enExample)

Families Citing this family (25)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
BRPI0406761A (pt) 2003-01-14 2005-12-20 Arena Pharm Inc Derivados de arila e heteroarila 1,2,3-trissubstituìdos como moduladores do metabolismo e a profilaxia e tratamento de distúrbios relacionados a estes tais como diabetes e hiper-glicemia
EP2108960A1 (en) 2008-04-07 2009-10-14 Arena Pharmaceuticals, Inc. Methods of using A G protein-coupled receptor to identify peptide YY (PYY) secretagogues and compounds useful in the treatment of conditons modulated by PYY
US20130109703A1 (en) 2010-03-18 2013-05-02 Boehringer Ingelheim International Gmbh Combination of a GPR119 Agonist and the DPP-IV Inhibitor Linagliptin for Use in the Treatment of Diabetes and Related Conditions
SG188548A1 (en) 2010-09-22 2013-04-30 Arena Pharm Inc Modulators of the gpr119 receptor and the treatment of disorders related thereto
WO2012135570A1 (en) * 2011-04-01 2012-10-04 Arena Pharmaceuticals, Inc. Modulators of the gpr119 receptor and the treatment of disorders related thereto
US8957062B2 (en) 2011-04-08 2015-02-17 Merck Sharp & Dohme Corp. Substituted cyclopropyl compounds, compositions containing such compounds and methods of treatment
WO2012170702A1 (en) * 2011-06-08 2012-12-13 Arena Pharmaceuticals, Inc. Modulators of the gpr119 receptor and the treatment of disorders related thereto
WO2012170867A1 (en) 2011-06-09 2012-12-13 Rhizen Pharmaceuticals Sa Novel compounds as modulators of gpr-119
WO2012173917A1 (en) 2011-06-16 2012-12-20 Merck Sharp & Dohme Corp. Substituted cyclopropyl compounds, compositions containing such compounds, and methods of treatment
EP2760855B1 (en) * 2011-09-30 2017-03-15 Merck Sharp & Dohme Corp. Substituted cyclopropyl compounds, compositions containing such compounds as well as their use in treating type-2 diabetes
US9018200B2 (en) 2011-10-24 2015-04-28 Merck Sharp & Dohme Corp. Substituted piperidinyl compounds useful as GPR119 agonists
WO2013062835A1 (en) * 2011-10-24 2013-05-02 Merck Sharp & Dohme Corp. Substituted piperidinyl compounds useful as gpr119 agonists
US9018224B2 (en) 2011-11-15 2015-04-28 Merck Sharp & Dohme Corp. Substituted cyclopropyl compounds useful as GPR119 agonists
CA2867114C (en) * 2012-06-12 2016-02-23 Chong Kun Dang Pharmaceutical Corp. Piperidine derivatives for gpr119 agonist
EP2872127A1 (en) 2012-07-11 2015-05-20 Elcelyx Therapeutics, Inc. Compositions comprising statins, biguanides and further agents for reducing cardiometabolic risk
WO2014052619A1 (en) * 2012-09-27 2014-04-03 Irm Llc Piperidine derivatives and compositions as modulators of gpr119 activity
RU2642429C2 (ru) * 2013-11-26 2018-01-25 Чон Кун Тан Фармасьютикал Корп. Амидные производные в качестве агонистов grp119
KR101651505B1 (ko) * 2014-05-02 2016-08-29 현대약품 주식회사 싸이클로 헥센 유도체, 이의 제조방법 및 이를 유효성분으로 함유하는 대사성 질환의 예방 또는 치료용 약학적 조성물
AU2016205361C1 (en) 2015-01-06 2021-04-08 Arena Pharmaceuticals, Inc. Methods of treating conditions related to the S1P1 receptor
CA3002551A1 (en) 2015-06-22 2016-12-29 Arena Pharmaceuticals, Inc. Crystalline l-arginine salt of (r)-2-(7-(4-cyclopentyl-3-(trifluoromethyl)benzyloxy)-1,2,3,4-tetrahydrocyclo-penta[b]indol-3-yl)acetic acid(com pound 1)for use in s1p1 receptor-associated disorders
CA3053418A1 (en) 2017-02-16 2018-08-23 Arena Pharmaceuticals, Inc. Compounds and methods for treatment of primary biliary cholangitis
CA3102136A1 (en) 2018-06-06 2019-12-12 Arena Pharmaceuticals, Inc. Methods of treating conditions related to the s1p1 receptor
TW202140440A (zh) 2020-02-28 2021-11-01 美商克力歐普股份有限公司 Gpr40激動劑
AU2021275038A1 (en) 2020-05-19 2022-12-22 Kallyope, Inc. AMPK activators
CA3183575A1 (en) 2020-06-26 2021-12-30 Iyassu Sebhat Ampk activators

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2008025798A1 (en) * 2006-08-30 2008-03-06 Biovitrum Ab (Publ) Pyridine compounds for treating gpr119 related disorders
WO2009038974A1 (en) * 2007-09-20 2009-03-26 Irm Llc Compounds and compositions as modulators of gpr119 activity

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
BRPI0406761A (pt) * 2003-01-14 2005-12-20 Arena Pharm Inc Derivados de arila e heteroarila 1,2,3-trissubstituìdos como moduladores do metabolismo e a profilaxia e tratamento de distúrbios relacionados a estes tais como diabetes e hiper-glicemia
US7638541B2 (en) * 2006-12-28 2009-12-29 Metabolex Inc. 5-ethyl-2-{4-[4-(4-tetrazol-1-yl-phenoxymethyl)-thiazol-2-yl]-piperidin-1-yl}-pyrimidine

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2008025798A1 (en) * 2006-08-30 2008-03-06 Biovitrum Ab (Publ) Pyridine compounds for treating gpr119 related disorders
WO2009038974A1 (en) * 2007-09-20 2009-03-26 Irm Llc Compounds and compositions as modulators of gpr119 activity

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
Bioisosterism A Rational Approach in Drug Design;George A. Patani, et al;《Chem. Rev.》;19961231;第96卷(第8期);3147-3176 *

Also Published As

Publication number Publication date
MA33428B1 (fr) 2012-07-03
MX2012000704A (es) 2012-03-07
CA2764906C (en) 2014-06-10
CR20120012A (es) 2012-03-28
EA201270169A1 (ru) 2012-06-29
JP5715127B2 (ja) 2015-05-07
ZA201200227B (en) 2013-06-26
NZ597125A (en) 2013-08-30
TW201114757A (en) 2011-05-01
IL216776A0 (en) 2012-03-01
JP2012533546A (ja) 2012-12-27
SG177646A1 (en) 2012-02-28
TWI429634B (zh) 2014-03-11
KR101365854B1 (ko) 2014-02-21
KR20120024964A (ko) 2012-03-14
CO6480977A2 (es) 2012-07-16
AU2010273642A1 (en) 2012-01-19
TN2012000002A1 (en) 2013-09-19
CA2764906A1 (en) 2011-01-20
WO2011008663A1 (en) 2011-01-20
AR077638A1 (es) 2011-09-14
AU2010273642B2 (en) 2014-03-13
EP2454251A1 (en) 2012-05-23
BRPI1015921A2 (pt) 2016-04-26
CN102471313A (zh) 2012-05-23
US8207344B2 (en) 2012-06-26
ECSP12011606A (es) 2012-02-29
DOP2012000006A (es) 2012-01-31
EA020540B1 (ru) 2014-11-28
PE20121045A1 (es) 2012-08-09
US20110015199A1 (en) 2011-01-20

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SE01 Entry into force of request for substantive examination
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CF01 Termination of patent right due to non-payment of annual fee

Granted publication date: 20140604

Termination date: 20160712